DMAPT

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DMAPT

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

870677-05-7

Dimethylamino Parthenolide

DMAPT (Dimethylamino Parthenolide) 是Parthenolide (PTL) 的类似物，是具有口服活性的NF-κB抑制剂，对原发性急性髓性白血病细胞的LD₅₀值为1.7 μM。具有潜在的抗肿瘤和抗转移作用。

生物活性

DMAPT (Dimethylamino Parthenolide), an analogue of Parthenolide (PTL), is an oral activeNF-κBinhibitor, with a LD₅₀of 1.7 μM for cell population in AML cells. Has potential anti-cancer and anti-metastatic effect^[1].

IC₅₀& Target

NF-κB^[1].

体外研究
(In Vitro)

DMAPT treatment decreased constitutive NF-κB binding activity, inhibits cell proliferation and viability of PC-3 and DU145 cells^[2].
Treatment of PC-3 and DU145 cells with 5 and 4 μM DMAPT, respectively, increases the population doubling times of PC-3 prostate cancer cells from 23.0 ± 5.0 h to 42.0 ± 3.0 h and of the DU145 cells from 20.4 ± 2.2 h to 72.5 ± 24.8 h^[2].

Cell Proliferation Assay^[2]

Cell Line:	PC-3 and DU145 cells.
Concentration:	PC-3 cells (0, 2.5, 5 μM), DU145 cells (0 and 4 μM).
Incubation Time:	24 and 48 hours.
Result:	Decreased constitutive NF-κB binding activity, inhibits cell proliferation and viability of PC-3 and DU145 cells.

体内研究
(In Vivo)

Treatment with DMAPT (100 mg/kg, Oral gavage daily for 7 days) increases sensitivity of PC-3 tumor xenografts to X-rays^[2].
DMAPT (100 mg/kg, Oral gavage thrice weekly from 42 to 300 days since birth) treatment slows normal tumor development in TRAMP mice, extending the time-to-palpable prostate tumor by 20%^[3].
DMAPT further reduces the metastatic area below that of the water vehicle treatment group in lung tissues (0.10% ± 0.15 SD, 92% reduction, p = 0.0028) in TRAMP mice^[3].

Animal Model:	PC-3 tumor xenograft in athymic nude mice^[2].
Dosage:	100 mg/kg.
Administration:	Oral gavage daily for 7 days.
Result:	Increased sensitivity of PC-3 tumor xenografts to X-rays.

Animal Model:	Six-week-old male TRAMP mice^[3].
Dosage:	100 mg/kg.
Administration:	Oral gavage thrice weekly from 42 to 300 days since birth.
Result:	Slowed normal tumor development in TRAMP mice, extending the time-to-palpable prostate tumor by 20%.

分子量

293.40

性状

Solid

Formula

C₁₇H₂₇NO₃

CAS 号

870677-05-7

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : 125 mg/mL(426.04 mM;Need ultrasonic)

H₂O : 1.1 mg/mL(3.75 mM;ultrasonic and warming and heat to 40℃)

配制储备液

浓度溶剂体积质量

1 mg

5 mg

10 mg

1 mM	3.4083 mL	17.0416 mL	34.0832 mL
5 mM	0.6817 mL	3.4083 mL	6.8166 mL
10 mM	0.3408 mL	1.7042 mL	3.4083 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.
请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline
Solubility: ≥ 2.08 mg/mL (7.09 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (7.09 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH2O 中，得到澄清透明的生理盐水溶液
2.
请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline)
Solubility: ≥ 2.08 mg/mL (7.09 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (7.09 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.
请依序添加每种溶剂： 10% DMSO 90%corn oil
Solubility: ≥ 2.08 mg/mL (7.09 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (7.09 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在本网站选购。